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Imidazo[2,1-b]thiazole guanylhydrazones as RSK2 inhibitors [1]

  1. Author:
    Andreani, A.
    Granaiola, M.
    Leoni, A.
    Locatelli, A.
    Morigi, R.
    Rambaldi, M.
    Varoli, L.
    Lannigan, D.
    Smith, J.
    Scudiero, D.
    Kondapaka, S.
    Shoemaker, R. H.

  2. Author Address

    [Andreani, A; Granaiola, M; Leoni, A; Locatelli, A; Morigi, R; Rambaldi, M; Varoli, L] Univ Bologna, Dipartimento Sci Farmaceut, I-40126 Bologna, Italy. [Lannigan, D] Univ Virginia, Dept Microbiol, Ctr Cell Signaling, Charlottesville, VA 22908 USA. [Smith, J] Univ Virginia, Dept Pathol, Ctr Cell Signaling, Charlottesville, VA 22908 USA. [Scudiero, D] NCI, SAIC Frederick, Frederick, MD 21702 USA. [Kondapaka, S; Shoemaker, RH] NCI, Screening Technol Branch, Dev Therapeut Program, Div Canc Treatment & Diag, Frederick, MD 21702 USA.;Andreani, A (reprint author), Univ Bologna, Dipartimento Sci Farmaceut, Via Belmeloro 6, I-40126 Bologna, Italy;aldo.andreani@unibo.it shoemakr@mail.nih.gov
    1. Year: 2011
    2. Date: Sep
  2. Journal: European Journal of Medicinal Chemistry
    1. 46
    2. 9
    3. Pages: 4311-4323
  4. Type of Article: Article
  5. ISSN: 0223-5234
  1. Abstract:

    The activity of a series of imidazo[2,1-b]thiazole guanylhydrazones as inhibitors of p90 ribosomal S6 kinase 2 (RSK2) is described. It was found that a small subset of compounds show both potent inhibition of RSK2 kinase activity and tumor cell growth in vitro. Detailed study of one of the most active compounds indicates a high degree of selectivity for inhibition of RSK2 compared to a spectrum of other related kinases. Selective inhibition of the MCF-7 breast tumor cell line compared to MCF-10A non-transformed cells, as well as selective inhibition of the biomarker GSK3 provides evidence that the compounds can affect the RSK2 target in cells. (C) 2011 Elsevier Masson SAS. All rights reserved.

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External Sources

  1. View Full Text
  2. DOI: 10.1016/j.ejmech.2011.07.001
  3. View record in Web of Science®
  4. WOS: 000295237400084

Library Notes

  1. Fiscal Year: FY2011-2012
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